Chemotherapy remains a cornerstone of cancer therapy and is widely employed in clinical practice. However, the therapeutic effect of chemotherapy is often hindered by drug resistance and adverse effects. Recent studies have highlighted the potential of ginseng active ingredients in combination with chemotherapy. This review systematically summarizes that ginseng active ingredients can not only inhibit tumor proliferation by promoting cancer cell apoptosis and arresting cancer cell cycle, inhibit tumor metastasis by suppressing epithelial-mesenchymal transition (EMT) and angiogenesis at the tumor site, but also reverse drug resistance by suppressing intracellular drug efflux and tumor immune evasion, and at the same time they can alleviate organ toxicities including nephrotoxicity, hepatotoxicity, cardiotoxicity, gastrointestinal toxicity, and ototoxicity as well as toxicities to the nervous system, hematopoietic system, and immune system induced by chemotherapy through multiple mechanisms, which shows great promise in cancer therapy. It elaborates the pharmacological actions of key constituents including ginsenoside Rg3 and Rh2, while incorporating innovative research findings on constituents including pseudoginsenoside F11, ginseng polysaccharides, and lipids. Furthermore, this review also specifically focuses on cutting-edge mechanisms including ferroptosis and pyroptosis, which enriches the theoretical basis of the application of ginseng active ingredients in cancer therapy and provides novel research directions.
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